Highland Pharmacy, Inc.

Estrogens

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A woman's body contains 3 natural estrogens:  Estrone (E-1), Estradiol (E-2), and Estriol (E-3).  Following is information regarding the use and dosage of estriol and estradiol each individually, and then a description of what a Biestrogen is and why it is used. 
 
 
ESTRIOL (E-3)
 
ESTRIOL is one of the three active estrogens found in the female body. Estriol is the dominant estrogen during pregnancy.  Estriol is a converted estrogen and is the end metabolite of both estradiol and estrone metabolism.  Estriol is considered by many to be the "forgotten" estrogen. It has been labeled in the U.S. as a weak or ineffective estrogen, while in Europe, estriol has been recognized for its benefits and has been used for years.

Estriol has a much less stimulating effect on the breast tissue and the uterine lining than both estradiol and estrone.  Estradiol is 1000 times more stimulating to the breast tissue than estriol.  Since estriol is the weakest of the three naturally occurring estrogens when it comes to estrogen activity, yet comprises nearly 80% of the total free estrogen in the female body, estriol is thought to have a protective effect in the female body.  That is, when estriol levels become low, there is less of this weak estrogen to occupy estrogen receptor sites, therefore leaving more estrogen sites available to be stimulated by the stronger estrogens, estradiol and estrone.  
 
Some researchers believe that not only does estriol NOT promote breast cancer, but it actually protects against the disease.  In 1966, H.M. Lemon, M.D. demonstrated that women with breast cancer have lower estriol levels.  He later showed that women without breast cancer had naturally higher estriol levels than those with breast cancer.
 
Estriol is the weakest of the three estrogens when used topically and orally, but considered the strongest when used locally to the vaginal canal.  Therefore, is thought to be a preferred estrogen when used vaginally.  When using low doses of estriol, no significant uterine or breast stimulation is typically observed.  Therefore, estriol is sometimes used in the high-risk patient where estrogen therapy needs to be extremely conservative.
 
Since little research has been completed, estriol has not conclusively shown the same positive protective effects to the heart in terms of raising HDL levels and maintaining bone mass as estradiol. Because of its weak action in the body, it sometimes fails to control many of the symptoms of menopause. It is for this reason that we see it used in combination with estradiol most frequently. Many women, however, do use estriol in combination with natural progesterone, and find the combination to be very successful.

Estriol, when used as a vaginal preparation for vaginal dryness and irritation, works incredibly well, without usually using any breast stimulation or uterine proliferation. For the high-risk patient, we reduce the strength down to .5mg per gram. The normal strength is 1-2mg per gram of gel. We generally recommend using for 7-10 consecutive days at bedtime, then use 2-3 times a week as symptoms dictate.
 
WHY USE ESTRIOL?
 
The key to the success of any hormone replacement therapy (HRT) program is the balancing of the body's natural hormone levels so that they will mimic the normal physiologic hormonal levels for that specific person.  Many times, different natural hormone (NH) compounds are prescribed as a matter of practitioner preference or personal good luck or experience with a preparation.  Certainly not to be overlooked is patient preference.  Through patient education, people have developed their own ideas on how they wish their HRT program to be structured.  Estriol is usually prescribed or more often requested by the patient because of the reputation it has developed as being a safe estrogen. 
 
MOST COMMON STRENGTHS
 
1 and 2mg      (2mg is thought to be equal to .625 mg conjugated estrogen)  We disagree.....it usually takes much more than 2mg of estriol to be equal to a .625mg conjugated estrogen. 
 
***Doses should always be individualized.*** We have over 900 formulas to choose from.***
 
**References for general information about natural hormones provided upon request.
 
 
 
ESTRADIOL(E-2)
 
ESTRADIOL is the strongest of the three naturally occurring estrogens found in the female body.  It is the most important and significant estrogen throughout a woman's productive life.  Estradiol is the most effective of the three estrogens.  It is primarily produced by the ovaries.  When we speak of the benefits of estrogen, most generally we think of estradiol as the main participant.  It is the most potent, and also the most beneficial estrogen in controlling all the estrogen deficient symptoms associated with menopause.  Estradiol is also recognized to be the most significant estrogen in raising high-density lipoproteins (HDL- the good cholesterol), maintaining bone mass, possible protection from Alzheimer's disease, improved skin, and many more.  Because of its relative activity compared to the other estrogens, estradiol can also be blamed for many estrogen-dominant characteristics, such as uterine proliferation, breast stimulation and tenderness, breast cancer, fluid retention, increased body fat, and reduced thyroid function, to mention a few.  Most, if not all, of these undesirable estrogen-dominant characteristics can be overcome with the proper balance of the natural estrogens, and the use of natural progesterone along with the estrogen therapy.
 
At this time, Estradiol is the only natural estrogen which is produced and sold commercially by drug companies.  The exception might be an occasional estrone injection product which seems to go on and off the market from time to time.  Estradiol is commercially available in tablet, patch, and vaginal form.  A commercial hybrid of estradiol, ethinyl-estradiol, is not a natural (bio-identical) hormone. 
 
Estradiol patches are thought by some endocrinologists to release medication sporadically thus causing irradic dosing and responses.  The biggest problem with the patch has traditionally been the adhesives used to attach them to the body.  Many women are allergic and develop sensitivites to the adhesives.  Many women find them hard to keep on their bodies while bathing. 
 
It is now believed that oral estrogens might reduce the production of growth hormone in women, thus indicating the topical route to be the best way of administering estrogen.
 
Estradiol when administered orally causes high levels of estrone to accumulate in the blood.  Some of the metabolites of estrone are known to be a problem.  When administered orally, Estradiol also decreases the conversion of T4 (the inactive form of thyroid) to T3 (the active form of thyroid), thereby reducing thyroid function.  In addition, oral Estradiol has also shown to increase insulin resistance.  When taken orally, estradiol may be more responsible for clot formation when compared to topically applied estradiol. 
 
 
WHY USE ESTRADIOL?
 
The key to the success of any hormone replacement therapy (HRT) program is the balancing of the bodies natural hormone levels so that they will mimic the normal physiologic hormonal levels for that specific person.  Estradiol is the primary estrogen produced by the body which metabolizes to both estrone and estriol.  It is easy to understand that an estrogen that converts or is metabolized to another estrogen might easily be out of balance if it is no longer being produced by the ovaries due to menopause.  Estradiol, as the strongest and most significant estrogen in the female body, has a proven track record as the most beneficial estrogen to control the symptoms of menopause, plus has the all the preventive effects enjoyed by estrogen.  Through the use of natural progesterone with estrogen therapy, most unwanted side effects of estrogen can be eliminated. 
 
MOST COMMON STRENGTHS
 
.5mg, 1mg, and 2mg.   
 
***Doses should always be individualized.*** We have over 900 formulas to choose from.***
 
**References for general information about natural hormones provided upon request.
 
 
WHY USE A BI-ESTROGEN?
 
Biestrogen, as the word might indicate, is a combination of two estrogens: Estriol (E-3), and Estradiol  (E-2). These two estrogens are 2 of the 3 natural occurring or "bio-identical" estrogens found in the female body.
 
BI-ESTROGEN= ESTRIOL + ESTRADIOL
 
The key to the success of any hormone replacement therapy (HRT) program is the balancing of the body's natural hormone levels so that they will mimic the normal physiologic hormonal levels for that specific person.  Many times, different natural hormone (NH) compounds are prescribed as a matter of practitioner preference or personal good luck or experience with a preparation.  Certainly not to be overlooked is patient preference.  Through patient education, people have developed their own ideas on how they wish their HRT program to be structured.   When a woman enters menopause, Estrone (E-1) the third estrogen, becomes dominant as the ovaries stop producing estradiol.  Estrone at this time is produced by the adrenals and in the fat tissue of the body.  Because estrone can be produced in the fat tissue of the body, depending on an individual (overweight) and diet, estrone levels can remain high.  It would then make sense if we have an abundance of estrone at menopause, we might choose to suppliment with only Estriol and Estradiol (thus bi-estrogen) to maintain proper balance of the body's natural hormones.  Remember, the balance of these hormones to each other is the key to a successful HRT program.
 
MOST COMMON STRENGTHS
 
1.25 mg and 2.5 mg
(2.5 mg given orally  twice a day is approximately equal to .625 mg of conjugated estrogen)
 
***Doses should always be individualized. We have over 900 formulas to choose from.***
 
STRENGTH TRANSLATION
 
There is NO general rule for a bi-estrogen:  Bi-estrogen = estriol + estradiol
 
Example:  Bi-est   2.5mg  =  2mg  estriol  +  .5mg  estradiol
Bi-est   2/1mg  =  2mg  estriol  +  1mg estradiol

The first number in  the strength designation is always ESTRIOL and the second number after the decimal (.) or back-slash (/) is always ESTRADIOL.
 
 
 
SOURCE OF NATURAL (BIO IDENTICAL) ESTROGENS
 
We compound all of our hormonal preparations using only all natural (bio-identical), soy (plant derived), USP grade, micronized hormone powders. When we say bio-identical, we mean exactly like the human body produces.  We use no animal products.  These products must not be confused with phyto (plant) products, which may mimic to a small degree some of the body's own hormones, but are not considered to be bio-identical hormones.  All of our compounded preparations require a prescription from a licensed practitioner.
 
SOME OF THE EFFECTS OF TOO MUCH ESTROGEN IN WOMEN
    • Uterine bleeding
    • Tender swollen breasts
    • Water retention
    • Increased body fat
    • Headaches
    • Hypertension
    • Irritability

Although these are general symptoms of too much estrogen, ESTRIOL generally does not display these symptoms unless prescribed in large doses. 

 
COMPOUNDED PREPARATIONS AVAILABLE
 
Oral capsules:  Made using natural gelatin capsules with hormone suspended in a cold pressed natural safflower oil with viamin E added.  Oil-filled oral capsules are known to give the best absorption of oral hormones.  For best absorption, capsules should be taken with food.  These preparations usually give more consistent results when dosed twice a day.
 
Topical gels:  Made using a base known as a hydro-alcoholic gel.  USP alcohol is added for stability and efficacy.  The gel base contains no oils, no petroleum additives, and no perfumes.  This type of base has been used in Europe for years as an industry standard known to be the best for delivery of topically applied hormones.  The strength of gels designated as mgs per 1/4 teaspoonful should be applied to inner arms or inner thighs; NO neck, face or mucous membranes.  Apply at least three consecutive days to one area for better tissue saturation and better results.  This should be dosed twice a day, if possible, to give more consistent results.  The little dose spoons we supply with topical preparations measure 1/8 teaspoonful when leveled off.
 
Vaginals:  Made using either a gel base or vanishing cream base.  This can be applied via an applicator or finger dab.  Generally women do not need a high introduction in the vaginal canal,  and therefore, a finger dab may be more convenient.
 
Combinations:  Progesterone, Testosterone, or DHEA may be added to any formula upon order from a practitioner. (Exception: we do not typically add these hormones to the vaginal preparations.)
 
 
**References for more information about natural hormones are provided upon request.
 
 

Highland Pharmacy, Inc.  717 Encino Place NE,  Albuquerque, NM 87102  505-243-3777
1-800-305-0405
email: highrx@rt66.com


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